Plural 1,2-diazoles (including Hydrogenated) Patents (Class 548/365.1)
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Patent number: 10556868Abstract: The present invention relates to a method for synthesizing a compound of 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid, wherein including the steps of: (A) the diethyl ester compounds represented by the following Formula IV are reacted under the action of amine, alkali and carbonyl reagents to produce the acrylic diester compound represented by the following Formula I, wherein: (B) the above compound represented by the Formula I is reacted with a fluoride reagent, a Lewis acid and a methyl hydrazine to form a pyrazole ring-containing diester compound represented by the Formula II, (C) the heterocyclic-containing diester compound represented by the Formula II is reacted with a base to give 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid represented by the Formula III.Type: GrantFiled: September 29, 2016Date of Patent: February 11, 2020Assignee: ZHEJIANG YONGTAI TECHNOLOGY CO., LTD.Inventors: Renbao He, Yingmei Wang, Hongming Shao, Yizhong Jin
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Publication number: 20150148373Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: June 7, 2013Publication date: May 28, 2015Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
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Publication number: 20150112075Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Carl DeAMICIS, Kaitlyn GRAY, Yu ZHANG, Joseck M. MUHUHI
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Patent number: 8975254Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 27, 2010Date of Patent: March 10, 2015Assignee: Orion CorporationInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Patent number: 8940273Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.Type: GrantFiled: January 15, 2013Date of Patent: January 27, 2015Assignee: Mallinckrodt LLCInventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
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Publication number: 20140378474Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: January 25, 2013Publication date: December 25, 2014Applicant: NOVARTIS AGInventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
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Publication number: 20140364621Abstract: This disclosure concerns two novel electrically conducting organic oligomers: oligo(3-amino-1H-pyrazole-4-carbonitrile) or “oligo(AP-CN)” and oligo(4-nitro-1H-pyrazole-3-yl-amine) or “oligo(AP-NO2)”, and methods of making thereof.Type: ApplicationFiled: May 16, 2014Publication date: December 11, 2014Applicant: The Government of the United States of America, as represented by the Secretary of the NavyInventors: Brett D. Martin, Scott A. Trammell, Jeffrey R. Deschamps, Jawad Naciri, Jeffrey C. DePriest
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Patent number: 8883689Abstract: A herbicide composition includes a fenoxaprop ester and a weak acid buffer system. The buffer system maintains the herbicidal composition at a pH in the range of 4 to 8. In one non-limiting embodiment, the fenoxaprop ester is fenoxaprop ethyl. The buffer system can include an amine-containing material, such as a tertiary amine. The herbicide composition can include other herbicides, such as weak acid herbicides, for example pyrasulfotole, bromoxynil, and/or bromoxynil esters and can include one or more safeners.Type: GrantFiled: August 24, 2006Date of Patent: November 11, 2014Assignee: Bayer CropScience LPInventors: Tai-Teh Wu, Karen L. Eagles
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Publication number: 20140303372Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: ApplicationFiled: March 28, 2014Publication date: October 9, 2014Applicant: ABBVIE BHAMAS LTD.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
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Publication number: 20140296238Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 10, 2014Publication date: October 2, 2014Inventors: Henry YU, Thomas E. RICHARDSON, Robert James FOGLESONG, Lizbeth Celeste DESELM, Andreas GOUTOPOULOS
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Publication number: 20140256771Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: October 19, 2012Publication date: September 11, 2014Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
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Publication number: 20140179733Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Publication number: 20140171420Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 6, 2013Publication date: June 19, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Pingchen Fan, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang, Dean Dragoli
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Patent number: 8716485Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.Type: GrantFiled: March 23, 2011Date of Patent: May 6, 2014Assignee: Westfälishe Wilhelms-Universität MünsterInventors: Julia Neumann, Mamta Suri, Frank Glorius
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Patent number: 8642508Abstract: The present invention is directed to the discovery, isolation, identification and methods of synthesis of a novel chemical complex that can be used to stabilize mixtures of different chemical compounds, and in particular mixtures of different herbicidal compounds.Type: GrantFiled: July 11, 2008Date of Patent: February 4, 2014Assignee: Bayer Cropscience LPInventors: Tai-Teh Wu, Karen L. Eagles, Michael W. Edenfield
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Publication number: 20140005231Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein L is —C(R12a)R12b—C(R13a)R13b—, wherein the carbon atom bonded to R12a and R12b is also bonded to the carboxamide nitrogen atom in Formula 1; or 1,2-phenylene optionally substituted with up to 4 substituents independently selected from halogen and C1-C2 alkyl; and A, Z, R1, R2, n, G and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are methods for controlling a phytophagous nematode comprising contacting the nematode or its environment with a nematocidally effective amount of a compound of Formula 1 wherein L is —C(R12a)R12b—C(R13a)R13b; and A, Z, R1, R2, n, G and Q are as defined in the disclosure.Type: ApplicationFiled: June 19, 2013Publication date: January 2, 2014Inventors: JAMES FRANCIS BEREZNAK, Steven Gutteridge, Ravisekhara P. Reddy, Andrew Edmund Taggi, Matthew James Campbell, Moumita Kar, Johan A. J. Desaeger
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Publication number: 20130274227Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20130177529Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: November 15, 2012Publication date: July 11, 2013Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
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Patent number: 8481494Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 26, 2010Date of Patent: July 9, 2013Inventors: Thomas Schrader, Katrin Hochdörffer, Julia März-Berberich, Luitgard Nagel-Steger, Gal Bitan, Sharmistha Sinha
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Publication number: 20130165452Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: February 22, 2013Publication date: June 27, 2013Applicant: PFIZER INC.Inventor: Pfizer Inc.
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Publication number: 20130131327Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.Type: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Mallinckrodt LLCInventor: Mallinckrodt LLC
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Publication number: 20130059833Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.Type: ApplicationFiled: August 30, 2012Publication date: March 7, 2013Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Patent number: 8372379Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.Type: GrantFiled: November 23, 2007Date of Patent: February 12, 2013Assignee: Mallinckrodt LLCInventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
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Publication number: 20130012715Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.Type: ApplicationFiled: March 23, 2011Publication date: January 10, 2013Applicant: WESTFAELISCHE WILHELMS UNIVERSITAET MUENSTERInventors: Julia Neumann, Mamta Suri, Frank Glorius
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Publication number: 20120316150Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.Type: ApplicationFiled: June 18, 2012Publication date: December 13, 2012Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Publication number: 20120270795Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: January 26, 2010Publication date: October 25, 2012Inventors: Thomas Schrader, Katrin Hochdörffer, Julia März-Berberich, Luitgard Nagel-Steger, Gal Bitan, Sharmistha Sinha
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Publication number: 20120238752Abstract: Provided is a colored photosensitive curing composition useful for color filters in primary colors, including blue, green, and red, having a high molar absorption coefficient and allowing a reduction in film thickness and superior color purity and fastness. A colored photosensitive curing composition, comprising, as its colorant, a dipyrromethene-based metal complex compound obtained from a metal or metal compound and a dipyrromethene-based compound represented by the following Formula (I): wherein in Formula (I), R1 to R6 each independently represent a hydrogen atom or a substituent group; and R7 represents a hydrogen or halogen atom, or an alkyl, aryl or heterocyclic group.Type: ApplicationFiled: May 23, 2012Publication date: September 20, 2012Applicant: FUJIFILM CORPORATIONInventors: Yuki MIZUKAWA, Ryoji GOTO, Hideki TAKAKUWA, Masashi OGIYAMA, Toru FUJIMORI
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Publication number: 20120225867Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 27, 2010Publication date: September 6, 2012Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Patent number: 8227619Abstract: The invention relates to a process for the preparation of fungicidally active compounds such as tricyclic amine derivatives (I). The process involves coupling of a carboxylic 5 acid e.g. a compound of formula (II) with an aniline, e.g. a compound of formula (III) in the presence of a boronic acid catalystor an antimony catalyst (II)(III)(I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Het are defined in the specification.Type: GrantFiled: May 11, 2009Date of Patent: July 24, 2012Assignee: Syngenta LimitedInventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, George Robert Hodges
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Patent number: 8222410Abstract: Provided is an azo pigment represented by the following general formula (1), a tautomer of the azo pigment, and a salt or a hydrate thereof: wherein Q represents the non-metallic atoms necessary to complete a 5- to 7-membered heterocyclic group, W represents an alkoxy group, an amino group, an alkyl group, or an aryl group, X1 and X2 each independently represents a hydrogen, an alkyl group, an acyl group, an alkylsulfonyl group, or an arylsulfonyl group, R1 represents a hydrogen or a substituent, R2 represents a heterocyclic group, n represents an integer of from 1 to 4 and the general formula (1) represents a dimer formed through Q, W, X1, X2, R1, or R2 when n=2, a trimer formed through Q, W, X1, X2, R1, or R2 when n=3, and a tetramer formed through Q, W, X1, X2, R1, or R2 when n=4.Type: GrantFiled: March 5, 2009Date of Patent: July 17, 2012Assignee: FUJIFILM CorporationInventors: Keiichi Tateishi, Shinya Hayashi, Masaru Takasaki, Nobuo Seto
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Publication number: 20120108424Abstract: The present invention is directed to the discovery, isolation, identification and methods of synthesis of a novel chemical complex that can be used to stabilize mixtures of different chemical compounds, and in particular mixtures of different herbicidal compounds.Type: ApplicationFiled: July 11, 2008Publication date: May 3, 2012Inventors: Tai-Teh Wu, Karen L. Eagles, Michael W. Edenfield
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Patent number: 8168796Abstract: There are provided novel fluorescent agents, such as pyrazoline compounds represented by formula (I): (wherein R1, R2 and R3 are as defined in the specification), having an ethynyl group in the molecule, which have high absorptivity in the ultraviolet-visible short wavelength range (for example, 350 nm-420 nm).Type: GrantFiled: January 19, 2009Date of Patent: May 1, 2012Assignee: Nippon Chemical Works Co., Ltd.Inventors: Kazuhiko Mizuno, Hideyuki Takagaki, Hirokazu Iwahashi, Kaname Inoue
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Publication number: 20110245157Abstract: This invention provides for dimeric1-arylpyrazole compounds, of formulas (I), (II), and (III): or salts thereof, and the use of these compounds against ectoparasites such as insects, arthropods and acarina. The resulting compounds may be used in veterinary formulations such as, for example, spot-on and pour-on formulations, which may be used for treatment, controlling and preventing of parasitic infections in warm-blooded animals and birds.Type: ApplicationFiled: November 18, 2009Publication date: October 6, 2011Inventor: Charles Q. Meng
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Publication number: 20110230445Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 8008278Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 27, 2010Date of Patent: August 30, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Patent number: 8003650Abstract: Disclosed is a hydrazine compound represented by the formula (1) below, which has an excellent control activity against a harmful arthropod. (1) (In the formula, R1, R5, R6 and R7 represent a hydrogen atom or the like; R2 and R3 are bonded together at their ends to form a 5- to 8-membered ring together with two nitrogen atoms; R4 represents a halogen atom or the like; J represents 1-(3-chloro-2-pyridyl)-3-bromo-1H-pyrazol-5-yl group or the like; and M represents a hydrogen atom, an optionally halogenated C1-C6 alkyl group, or the like.Type: GrantFiled: April 10, 2008Date of Patent: August 23, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Markus Jachmann, Hiroshi Ikegami, Yoshihiko Nokura
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Patent number: 7994341Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.Type: GrantFiled: September 14, 2006Date of Patent: August 9, 2011Assignee: Syngenta LimitedInventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi, Fanny Giordano, Martin Zeller, Gottfried Seifert, Shailesh Shah, Neil George, Ian Kevin Jones, Paul Edward Bonnett
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Publication number: 20110144080Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: December 23, 2004Publication date: June 16, 2011Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITALInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Patent number: 7947680Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: July 17, 2009Date of Patent: May 24, 2011Assignee: H. Lundbeck A/SInventors: Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
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Publication number: 20110092539Abstract: The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: June 3, 2009Publication date: April 21, 2011Inventors: Jonathan Gillespie, Craig Jamieson, Zoran Rankovic
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Patent number: 7923004Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: GrantFiled: October 15, 2007Date of Patent: April 12, 2011Assignee: XTL Biopharmaceuticals Ltd.Inventors: Guolin Li, Reza Fathi, Zhen Yang, Yun Liao, Qiang Zhu, Angela Lam, Anthony Sandrasagra, Kenneth Nawoschik, Hyun-Joon Cho, Jie Cao, Wu Ruoqiu, C. Richard Wobbe, Yixin Liu
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Patent number: 7893611Abstract: There is provided a novel luminescent metal complex. A metal complex having a composition of [(PtII)2(MI)2(X)2(L)4(LH)2], where MI denotes AgI, AuI or CuI, X denotes Cl, Br or I, L denotes a structure represented by the formula (1), and LH denotes a structure represented by the formula (2).Type: GrantFiled: November 1, 2007Date of Patent: February 22, 2011Assignee: Nagasaki UniversityInventors: Keisuke Umakoshi, Seiji Akatsu, Masayoshi Onishi, Shoji Ishizaka, Noboru Kitamura
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Publication number: 20100249091Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally subsType: ApplicationFiled: September 17, 2009Publication date: September 30, 2010Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Publication number: 20100144793Abstract: The present invention relates to compounds of the general formula (I) wherein (formula 2) independently represents a single bond or a double bond, represents a linking group A and A? are each independently a 5- to 7-membered heterocyclic ring, wherein the heterocyclic rings A und A? are optionally substituted by one or more substituents, selected from C1-6 alkyl, C3-6 cycloalkyl, optionally substituted phenyl, optionally substituted heteroaryl, C1-4 alkylene-(optionally substituted phenyl) and C1-4 alkylene-(optionally substituted heteroaryl), or two substituents may be joined to form an optionally substituted, saturated, unsaturated or aromatic 5- to 7-membered ring which is fused with the heterocyclic ring A or A?, and wherein the heterocyclic rings A und A? may contain in addition to the units X, X?, Y and Y? one or more heteroatoms, selected from N, NR, S and Ol wherein R is selected from H and C1-4 alkyl; the units X and X? are each independently a H-bond acceptor; and the units Y and Y? are each indepenType: ApplicationFiled: November 23, 2007Publication date: June 10, 2010Applicant: AC IMMUNE SAInventors: Wolfgang Froestl, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas Muhs, Maria Pihlgren Bosch
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Patent number: 7728018Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: GrantFiled: September 21, 2007Date of Patent: June 1, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
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Patent number: 7696199Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: GrantFiled: August 29, 2005Date of Patent: April 13, 2010Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, María Montserrat Contijoch-Llobet
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Publication number: 20100074842Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.Type: ApplicationFiled: November 23, 2007Publication date: March 25, 2010Inventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
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Publication number: 20100063063Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: September 9, 2009Publication date: March 11, 2010Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 7662961Abstract: The invention relates to bis-5-pyrazolyl derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).Type: GrantFiled: December 22, 2006Date of Patent: February 16, 2010Assignee: Merial LimitedInventors: Stefan Schnatterer, Michael Maier, Friederike Lochhaas, Werner Knauf, Karl Seeger
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Patent number: 7592338Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: August 2, 2007Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski